A rational approach to the design and synthesis of a new bradykinin B1 receptor antagonist

P Bedos, M Amblard, G Subra, P Dodey…

Index: Bedos, Philippe; Amblard, Muriel; Subra, Gilles; Dodey, Pierre; Luccarini, Jean-Michel; Paquet, Jean-Luc; Pruneau, Didier; Aumelas, Andre; Martinez, Jean Journal of Medicinal Chemistry, 2000 , vol. 43, # 12 p. 2387 - 2394

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Citation Number: 32

Abstract

We have previously synthesized a potent and selective B1 bradykinin receptor antagonist, JMV1645 (H-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH), containing a dipeptide mimetic ((3 S)- amino-5-carbonylmethyl-2, 3-dihydro-1, 5-benzothiazepin-4 (5 H)-one (D-BT) moiety) at the C-terminal. Analogues of this potent B1 bradykinin receptor antagonist in which the central Pro2-Hyp3-Gly4-Igl5 tetrapeptide has been replaced by constrained N-1-substituted-1, 3, ...